Description
Emixustat, a novel visual cycle modulator, is an inhibitor of the visual cycle isomerase with an IC50 value of 4.4 nM in vitro.
Product information
CAS Number: 1141777-14-1
Molecular Weight: 263.38
Formula: C16H25NO2
Chemical Name: (1R)-3-amino-1-[3-(cyclohexylmethoxy)phenyl]propan-1-ol
Smiles: NCC[C@@H](O)C1C=CC=C(C=1)OCC1CCCCC1
InChiKey: WJIGGYYSZBWCGC-MRXNPFEDSA-N
InChi: InChI=1S/C16H25NO2/c17-10-9-16(18)14-7-4-8-15(11-14)19-12-13-5-2-1-3-6-13/h4,7-8,11,13,16,18H,1-3,5-6,9-10,12,17H2/t16-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 43 mg/mL (163.26 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Emixustat potently inhibits isomerase activity in vitro (IC50=4.4 nM). Treatment of emixustat shows a concentration dependent reduction of 11-cis-ROL production . Emixustat strongly inhibits 11-cis-retinol production with an IC50 value of 232±3 nM.
In Vivo:
Emixustat reduces the production of visual chromophore (11-cis retinal) in wild-type mice following a single oral dose (ED50=0.18mg/kg). In albino mice, emixustat is shown to be effective in preventing photoreceptor cell death caused by intense light exposure. Pre-treatment with a single dose of emixustat (0.3 mg/kg) provids a 50%protective effect against light-induced photoreceptor cell loss, while higher doses (1-3 mg/kg) are nearly 100%effective. In Abca4-/- mice, chronic (3 month) emixustat treatment markedly reduces lipofuscin autofluorescence and reduces A2E levels by 60%( ED50=0.47 mg/kg). In the retinopathy of prematurity rodent model, treatment with emixustat during the period of ischemia and reperfusion injury produces a 30%reduction in retinal neovascularization (ED50=0.46mg/kg).
Products are for research use only. Not for human use.
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